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Compounds, compositions, and methods for treatment of disease

A compound and an independent technology, applied in the direction of chemical instruments and methods, drug combinations, active ingredients of heterocyclic compounds, etc., can solve problems such as autoinflammatory disorders

Pending Publication Date: 2021-11-12
F STAR THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Furthermore, mutations in STING have been reported to lead to autoinflammatory disorders

Method used

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  • Compounds, compositions, and methods for treatment of disease
  • Compounds, compositions, and methods for treatment of disease
  • Compounds, compositions, and methods for treatment of disease

Examples

Experimental program
Comparison scheme
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example

[0340] The invention now generally described may be more readily understood by reference to the following examples, which are included for the purpose of illustrating certain aspects and embodiments of the invention only and are not intended to be limiting of the invention.

example 1

[0341] Example 1: Preparation of Exemplary Compounds of the Disclosure

[0342] method 1:

[0343]

[0344] To a solution of an appropriately substituted purine (2 mmol) and RBr / RCl / RI (2.5 mmol) in anhydrous DMF (5 mL) was added anhydrous potassium carbonate (3 mmol) and a few crystals of NaI. The suspension was heated slowly under argon in an oil bath at 65°C-70°C for 3h. The progress of the reaction was monitored on TLC using DCM-MeOH (2.5%). After the reaction was complete, the reaction mixture was cooled to room temperature and concentrated at 50 °C to remove most of the DMF. Hexanes (10 mL) were added and the remaining DMF was removed. The residue was partitioned between EtOAc (50 mL) and water (15 mL). The organic layer was separated, and the aqueous layer was re-extracted into EtOAc (25 mL). The combined organic layers were washed with water (15ml), sodium bicarbonate (5%, 2X 15mL) and then with saturated NaCl solution (10mL). The organic layer was washed ...

example 2

[0934] Example 2: Protocol for Testing STING Antagonistic Activity of Exemplary Compounds of the Disclosure in THP-1 and RAW Cells

[0935] Cells and Cell Culture Conditions

[0936] THP-1 double cells (InvivoGen) were incubated at 37°C in 5% CO 2 cultured in RPMI containing 10% fetal bovine serum (FBS), 100 IU mL-1 penicillin and 100 μg mL-1 streptomycin. RAW-ISG cells (InvivoGen) were incubated at 37 °C in 5% CO 2 cultured in DMEM containing 10% fetal bovine serum (FBS), 100 IU mL-1 penicillin and 100 μg mL-1 streptomycin. THP-1 double cells were seeded into 96-well assay plates on the day of the assay, while RAW cells were seeded into 96-well assay plates 18 hours before the assay.

[0937] Cell-based ISG54 promoter-reporter luciferase measurement of IRF activity in THP-1 double cells:

[0938] 50,000 cells seeded in 96-well flat-bottomed white assay plates were treated with compounds at different concentrations (10uM to 0.01uM) for 1 h, and then STING was induced wit...

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Abstract

Disclosed are compounds and compositions for inhibiting the expression of a pattern recognition receptor (e.g., STING), and methods of use thereof.

Description

[0001] related application [0002] This application claims the benefit of priority to U.S. Provisional Patent Application No. 62 / 879,178, filed July 26, 2019, and U.S. Provisional Patent Application No. 62 / 814,025, filed March 5, 2019; the contents of each are incorporated by reference in their The entire text is incorporated herein. Background technique [0003] Mammalian cells have evolved several intracellular sensors that recognize abnormal species (such as DNA) in the cytoplasm and trigger an innate immune response in response. Examples of these sensors include: endosomal Toll-like receptors, expressed in plasmacytoid dendritic cells (pDCs) and B cells; absence of melanoma 2 (AIM2), which recognizes double-stranded DNA (dsDNA) and induces pro- Activation of the inflammatory IL1b and IL18 cytokines; and Stimulator of Interferon Genes (STING), which binds to cyclic dinucleotides (CDNs) and leads to induction of interferon and NF-kβ signaling pathways. [0004] Another e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K31/4192C07D487/04
CPCC07D487/04C07D473/40C07D473/00C07D473/32C07D473/34C07D473/30C07D473/38C07D471/04C07D519/00C07F9/65616A61K31/52A61K31/437A61K31/5377A61P37/00A61P29/00A61P35/00A61P25/00A61P31/00A61P33/10A61P37/06A61K31/519A61K31/675
Inventor R·P·艾尔S·帕马纳班S·巴斯卡兰A·舍里D·克利里R·马斯特罗利亚S·周S·查拉R·H·吉米V·奈尔L·P·苏皮亚
Owner F STAR THERAPEUTICS INC
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